pimobendan Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
cardiac stimulants, pimobendan derivatives 2171 74150-27-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • UD-CG 115 BS
  • UDCG 115
  • pimobendan
  • acardi
produces arterial & venous dilatation in dogs; structure given in first source
  • Molecular weight: 334.38
  • Formula: C19H18N4O2
  • CLOGP: 2.90
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 79.37
  • ALOGS: -4.36
  • ROTB: 3

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 2 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 14 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1994 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cardiac failure 129.67 45.09 41 358 79907 46605756

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cardiac failure 118.13 38.88 50 619 83368 29868441
Cardiac failure chronic 42.45 38.88 12 657 5851 29945958

Pharmacologic Action:

SourceCodeDescription
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D010726 Phosphodiesterase Inhibitors
MeSH PA D020011 Protective Agents
MeSH PA D014665 Vasodilator Agents
CHEBI has role CHEBI:35620 vasodilator
CHEBI has role CHEBI:38147 cardiotonic drugs
CHEBI has role CHEBI:50218 phosphodiesterase inhibitors

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.86 acidic
pKa2 11.61 acidic
pKa3 4.76 Basic
pKa4 4.16 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Phosphodiesterase 3 Enzyme INHIBITOR IC50 6.39 CHEMBL SCIENTIFIC LITERATURE
Type-1 angiotensin II receptor GPCR IC50 4.77 CHEMBL

External reference:

IDSource
D01133 KEGG_DRUG
C0071071 UMLSCUI
CHEBI:32003 CHEBI
4823 PUBCHEM_CID
CHEMBL24646 ChEMBL_ID
DB11450 DRUGBANK_ID
C041648 MESH_SUPPLEMENTAL_RECORD_UI
5090 INN_ID
34AP3BBP9T UNII
1110783 RXNORM
017800 NDDF

Pharmaceutical products:

None